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1-(5-Carboxy- and 5-carbamoylindol-1-yl)propan-2-ones as inhibitors of human cytosolic phospholipase A2α: Bioisosteric replacement of the carboxylic acid and carboxamide moiety

Authors
Journal
Bioorganic & Medicinal Chemistry
0968-0896
Publisher
Elsevier
Publication Date
Volume
15
Issue
8
Identifiers
DOI: 10.1016/j.bmc.2007.02.016
Keywords
  • Cytosolic Phospholipase A2α Inhibitors
  • Indol-1-Ylpropan-2-Ones
  • Bioisosteric Replacement
Disciplines
  • Biology

Abstract

Abstract Indole-5-carboxylic acids and -carboxamides with 3-aryloxy-2-oxopropyl residues in position 1 were previously reported to be potent inhibitors of cytosolic phospholipase A 2α (cPLA 2α) isolated from human platelets. In continuation of our attempts to develop novel cPLA 2α inhibitors, a number of derivatives of these substances characterized by bioisosteric replacement of the carboxylic acid and carboxamide functionality, respectively, were prepared. The results of the biological evaluation of the obtained compounds enabled us to gain further insight into structural features critical for cPLA 2α inhibition.

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